Current Issue : October-December Volume : 2012 Issue Number : 4 Articles : 28 Articles
The concepts of particle engineering and dosage form design have become dominant themes in pharmaceutical manufacturing. The need for particle size con¬trol of pharmaceuticals is becom¬ing more important as the industry attempts to formulate active phar¬maceutical ingredients (API’s) with poor aqueous solubility, which constitutes up to 40% of new chemical entities. The fundamental issue with particle size analysis is the variety of equivalent particle diameters generated by different methods, which is largely ascribable to the particle shape and particle dispersion mechanism involved. Thus, to enable selection of the most appropriate or optimal sizing technique, cross-correlation between different techniques may be required....
A fast-dissolving drug delivery system, in most cases, is a tablet that dissolves or disintrigrants in the oral cavity without the need of water or chewing. Most fast-dissolving delivery system films must include substances to mask the taste of the active ingredient. This masked active ingredient is then swallowed by the patient''s saliva along with the soluble and insoluble excipients. These are also called melt-in-mouth tablets, repimelts, porous tablets, oro-dispersible, quick dissolving or rapid disintegrating tablets....
Fast-dissolving drug technologies are rapidly gaining interest in the pharmaceutical industry. These delivery systems either dissolve or disintegrate in the mouth rapidly, without requiring any water to aid in swallowing. Such technologies offer a convenient way of dosing medications, not only to special population groups with swallowing difficulties, but also to the general population. They also impart unique product differentiation, thus enabling use as line extensions for existing commercial products. This review discusses the various technologies used to achieve quick dissolution/dispersion in the oral cavity. They are categorized based on either processing or formulation variables. Processing techniques, such as Zydis, Quick-Dis, Soluleaves, Wafertab are discussed in this article. The oral mucosa has rich blood supply and it is relatively permeable. The permeability of the buccal mucosa is 4- 1000 time greater then that of skin. the administration of drugs by the oral route has several advantage over per oral administration such as QWICK ACTION, avoid of first pass metabolism , drug is not subject to acidic environment of the stomach and also the improved patient compliance particularly with pediatric & geriatric patient. It is the objective of this article to review the oral fast dissolving drug delivery such as fast dissolving/disintegrating film & tablet, fast dissolving capsule and medicated chew gum etc....
The Pioglitazone microcapsules were formulated with a view to improve the oral bioavailability and to attain the anti hyperglycemic effect within short period of time. The Pioglitazone microcapsules were formulated with Eudragit E100 by using coacervation phase separation technique. Microcapsules were evaluated for various parameters and subjected to the pharmacodynamic studies in healthy albino rabbits. The blood glucose levels were measured and the percent glucose reduction was calculated. The % blood glucose reduction observed from the pure drug and microcapsules was compared. The microcapsules exhibited the desired flow properties and higher dissolution rates. Microcapsules of Pioglitazone showed more anti hyperglycemic activity compared to pure drug....
The purpose of this study was to develop formulations and systematically evaluate in vitro performances of buccoadhesive bilayer patches of zolpidem tartrate. Backing layer was formulated using Ethylcellulose N10 as a hydrophobic polymer and 70% of triethylcitrate of dry polymer weight as a plasticizer for backing layer. The mucoadhesive polymer chitosan and hydrophilic polymer HPMC E15 were incorporated into the buccoadhesive patches, to provide bioadhesive properties to the patches and to modify the rate of drug release. The patches, which were prepared by the solvent casting method, were smooth and elegant in appearance; were uniform in thickness, weight, and drug content; showed no visible cracks; and showed good folding endurance. A 32 full factorial design was employed to study the effect of independent variables like mucoadhesive polymer chitosan and hydrophilic polymer HPMC E15, which significantly influenced characteristics like ex vivo mucoadhesive strength and in vitro drug release at different time points. A stability study of optimized buccoadhesive patches was done in natural human saliva; it was found that both drug and buccal patches were stable in human saliva. It can be concluded that the present buccal formulation can be an ideal system to improve the bioavailability of the drug by avoiding hepatic first-pass metabolism....
The field of dosage form designing and pharmaceutical modeling revels in the development of dosage forms that enhance bioavailability, in vivo stability, intestinal absorption and therapeutic efficacy on the whole. One such endeavor for a Novel drug delivery system is aquasome. Aquasomes are self assembling, tri-partied novel drug delivery systems that are also called as water bodies as their water like properties provides a platform for preserving the conformational integrity and bio chemical stability of bio-actives. Unique three-dimensional conformation, a freedom of internal molecular rearrangement induced by molecular interactions and a freedom of bulk movement are some of the key components of the system. Their mechanism of action is controlled by their surface chemistry as they deliver contents through combination of specific targeting, molecular shielding, and slow and sustained release process. Further due to their size and structure stability, avoid clearance by reticuloendothelial system or degradation by other environmental challenges. Structurally an aquasome comprises of a drug core situated on the outside lined by an Oligomeric carbohydrate nanocrystalline film. Another key feature is the presence of calcium phosphate di-hydrate, which is unstable and converts to hydroxyapatite upon prolong storage and is used for self assembling of the dosage form. The present paper reviews the dosage form pharmaceutically as well as enumerates biopharmaceutical applications and impinges the requirement of aquasomal drug delivery....
Among the dosage forms developed to facilitate ease of medication, the rapid disintegrating tablet (RDT) is one of the most widely employed commercial products. Swallowing problems also are common in young individuals because of their underdeveloped muscular and nervous systems. Other groups that may experience problems using conventional oral dosage forms In some cases such as motion sickness, sudden episodes of allergic attack or coughing, and an unavailability of water, swallowing conventional tablets may be difficult. The unique property of mouth dissolving tablet is that they are rapidly disintegrating and/or dissolving and release the drug as soon as they come in contact with saliva, thus obviate the requirement of water during administration. Fast dissolving tablets (FDTs) have received ever-increasing demand during the last decade, and the field has become a rapidly growing area in the pharmaceutical industry. Upon introduction into the mouth, these tablets dissolve or disintegrate in the mouth in the absence of additional water for easy administration of active pharmaceutical ingredients. The popularity and usefulness of the formulation resulted in development of several FDT technologies. These tablets readily dissolve or disintegrate in the saliva i.e. within less than 60sec without the need for water. They have been formulated for pediatric, geriatric and bedridden patients. This type of dosage forms are also ideal for active patients who are busy and traveling and may not have access to water....
The purpose of this study was to design matrix tablets of Paracetamol to overcome its side effects and to increase its bioavailability. Carnuba Wax and Bees Wax were used in matrix tablets at various concentrations for sustained drug delivery. Compression and flow properties of powder mixtures were tested before tablets were compressed by direct compression method. Weight variation, diameter and thickness, hardness, tensile strength, friability % and disintegration time of tablets were tested for their physical characterization. Determination method of drug in dissolution mediums was validated through spectroscopic method. All formulations met compendial requirements and any chemical interaction between drug and tablet excipients was not detected. It was observed that waxy tablets released drug faster than polymer based tablets. Waxy tablets generally displayed diffusionally controlled drug release....
The purpose of the present study was to develop an optimized matrix tablet of bupropion hydrobromide. The model drug is highly soluble in water and the matrix tablet of the same has shown drug release for 12 hours. The FTIR analysis shows that there is no significant interaction between drug and polymers used in the formulation. An augmented simplex centroid design was constructed for optimizing matrix tablets of bupropion hydrobromide, where the amounts of xanthan gum (X1), guar gum (X2) and sodium alginate (X3) were selected as the independent variables. Drug release at 12th h (Y1) and time required for 50% drug release (Y2) were selected as dependent variables. All other variables due to formulations and processing were kept invariant throughout the study. Results of evaluation of matrix tablet shows that, optimized formulation containing 3.33% of xanthan gum, 4.44 % of guar gum and 4.44 % of sodium alginate show 98.63±1.72 % drug release at 12th h and 50% drug release in 2.69±0.58 h. Swelling of the tablets increased with an increased amount of sodium alginate up to 8 h further the tablet starts to erode. All the gums contribute for the swelling behavior of the tablet and also help to maintain the integrity of tablet throughout the study....
The aim of present work was to develop a robust formulation of Bi-layer tablets of diclofenac sodium tablet. The basic aim of Bi-layer tablet formulation is to produce immediate action or prolonged action tablet. Wet granulation process was used for the formulation of matrix tablet layers and direct compression method process was used for the formulation of fast disintegrating layer of tablet. Tablets were evaluated for the thickness, weight variation, hardness, friability, disintegration time, dissolution study and compiled all the parameters with the official specifications. Based on the release kinetic parameters calculated, the drug contained in the fast disintegrating layer dissolved within the first 6 min & drug contained in the matrix layer dissolved upto 6 hr, so it can be concluded that tablets were particularly suitable for fast & long lasting action....
The objective of this study was to develop self-micro emulsifying drug delivery system (SMEDDS) to enhance the oral absorption of the poorly water-soluble drug, Efavirenz. The influence of the oil, surfactant and co-surfactant types on the drug solubility and their ratios on forming efficient and stable SMEDDS were investigated in detail. The SMEDDS were characterized by morphological observation, droplet size and zeta potential determination, freeze thawing and in vitro release study. The optimum formulation consisted of 45% Acconon MC-8 EP, 26.66% Cremophor EL and 13.33% Polyethylene glycol 400. In vitro release test showed a complete release of Efavirenz from SMEDDS in an approximately 4 h. The absorption of Efavirenz from SMEDDS showed increase in absorption compared with that of the marketed formulation. Our studies demonstrated the promising use of SMEDDS for the delivery of Efavirenz by the oral route....
Losartan Potassium is an angiotensin II receptor antagonist. It suppresses the effects of angiotensin II at its receptors, thereby blocking the rennin angiotensin system. The rennin angiotensin system plays a crucial role in hypertension. Sublingual tablets of Losartan Potassium were prepared to improve its bioavailability, to avoid pre-systemic metabolism in the gastrointestinal tract and hepatic first pass elimination. The Sublingual tablets were prepared by direct compression procedure using different concentration of Starch 1500 and microcrystalline cellulose. Compatibility studies of drug and polymer were performed by FTIR spectroscopy and DSC. Preformulation property of API was evaluated. Postcompressional parameters such disintegration time, wetting time, water absorption ratio, in vitro drug release and in vivo bioavailability study of optimized formulation were determined. TIR spectroscopy and DSC study revealed that there was no possible interaction between drug and polymers. The precompression parameters were in acceptable range of pharmacopoeial specification. The disintegration time of optimized formulation (F3) was upto 48 sec. The in vitro release of Losartan Potassium was upto 15 min. The percentage relative bioavailability of Losartan Potassium from optimized sublingual tablets was found to be 144.7 %. Sublingual tablets of Losartan Potassium were successfully prepared with improved bioavailability...
An attempt was made to formulate and evaluate the Gallic acid transdermal drug delivery system. Preformulation studies on the drug Gallic acid were done which included description, solubility and compatibility studies. The transdermal patches were made which were of matrix diffusion control system. Solvent casting technique was used to prepare the transdermal patches. Three formulations were made with 20mg of Gallic acid and by using polymers namely hydoxy propyl methyl cellulose, ethyl cellulose at various ratios and the yield was noted. Gallic acid was physically examined for color and odour. Solubility was determined in water, phosphate buffer pH -7.4, Ethanol, DMSO and Tetra hydro furan. Interaction of drug and polymer was confirmed by UV – Visible interaction and FTIR studies. Based on this further evaluation was carried out. Invitro drug diffusion stuy was also carried out using modified Franz diffusion cell.Transdermal patches were evaluated for the weight, thickness, percentage moisture uptake, percentage flatness, folding endurance, water vapor transmission rate, and in-vitro release studies. This was done for three formulations F1, F2, F3. It was found that formulation F1 showed the best compatibility on the basis of all tests performed....
The present study was carried out to formulate mouth dissolving dissolving tablets (MDTs) of Cyproheptadine HCl for enhanced solubility and dissolution profile in comparison to the marketed formulation. In our study, MDTs were prepared by Sublimation method using camphor, thymol and menthol as subliming agent. For solubility enhancement of Cyproheptadine HCl, solid dispersion with Poloxamer 407 was prepared and used in formulation. All the prepared formulations were evaluated for general appearance, physical parameters, drug content and In vitro drug release studies. The properties of all the formulations were found to be within the standard limits. All the MDTs get dispersed within a minutes when tested for In vitro dispersion. The In vitro drug release of MDTs (F7) shows good release with 45.4±0.17 % in 5 minutes, which increased up to 98.3±0.35% in 30 minutes in comparison to Marketed tablet which shows only 14.7±0.36% in 5 min. and fails to release more than 34.5±0.75% within 30 minutes....
Emulsions are successfully applied in many fields of human activity. Traditionally, emulsion have been defined as consisting of two liquids , of which one is dispersed in other as microscopic drops, stabilized by monomolecular layers of emulsifier at interface. But when these are used as colloidal carrier, the stability of emulsion droplets often requires much improvement. In recent times emulsion containing lipid droplets coated by nano-laminated layers are prepared by a simple cost effective method using food ingredients. Shelf life of cosmetic, pharmaceutical, and food formulations can be improved by increasing stability. Concerted efforts in future may direct us to newer approaches and ways for better usage of multilayer stabilized emulsion in human life....
Particle size specification of pharmaceutical powders is important in the manufacture of solid oral dosage forms due to significant impact of particle size on the safety and efficacy of the drug product so it should meet the regulatory requirement. In the manufacture of solid oral dosage forms, control of particle sizes is only taken into consideration for the drug substances with low solubility. Particle sizes of powders have clear influences on, not only drug product performance (e.g., dissolution, content uniformity and stability etc.) but also drug product manufacturability (e.g., flowability, blend uniformity, compactibility etc.). This Review article gives detailed information about how the particle size specifications are helpful in establishing drug product quality and manufacturing consistency, about the various methods for particle size specification such as Analytical Procedures, Method Validation, and Acceptance Criteria....
The in-vitro release characteristics of the class II active pharmaceutical ingredients according to Biopharmaceutical classification system are very slightly water soluble. The absorption rate of a poorly water-soluble drug, from the orally administered solid dosage form is controlled by its dissolution rate in the fluid present at the absorption site, i.e. the dissolution rate is often the rate-determining step in drug absorption. Among all newly discovered chemical entities about 40% drugs are lipophillic and fail to reach market due to their poor water solubility. The solubility behaviour of drugs remains one of the most challenging aspects in formulation development. Different methods are discussed here....
Nanotechnology has potential application in diagnosis, imaging and treatment of cancer. The different nanomedicine likes nanoshells, nanowires, superparamagnetic nanoparticles and a surface modified nanoparticle has been used in cancer treatment for targeted action. The nanowires are placed across microfludic channel which interact with molecular markers of cancer cells. Nanoscale cantilevers work depend on the semiconductor lithographic Techaniques. The cantilevers are coated by antibodies which interact with special molecules secreted by cancer cells. In now a day’s the potential toxicity of nanoparticles due to their smaller size related to human and enviourment are also of great concerned....
The purpose of writing this review on pulsatile drug delivery systems (PDDS) is to compile the recent literatures with special focus on the different types and approaches involved in the development of the formulation. PDDS are gaining importance in the field of pharmaceutical technology as these systems deliver the right dose at specific time at a specific site. Some of the disease conditions wherein PDDS are promising include duodenal ulcer, cardiovascular diseases, arthritis, asthma, diabetes, neurological disorder, cancer, hypertension and hypercholesterolemia. PDDS can be classified into time controlled systems wherein the drug release is controlled primarily by the delivery system, stimuli induced PDDS in which release is controlled by the stimuli, such as the pH or enzymes present in the intestinal tract or enzymes present in the drug delivery system and externally regulated system where release is programmed by external stimuli like magnetism, ultrasound, electrical effect and irradiation. This review also summarizes some current PDDS already available in the market. These systems are useful to several problems encountered during the development of a pharmaceutical dosage form....
Oral fast dissolving film (FDF) is one such novel approach to increase consumer acceptance by virtue of rapid dissolution, self administration without water or chewing. Oral fast dissolving film is relatively a new dosage form in which thin film is prepared using hydrophilic polymers, which rapidly dissolves on tongue or buccal cavity. The film is placed on the top or the floor of the tongue. It is retained at the site of application and rapidly releases the active agent for local and/or systemic absorption. Different polymers like Pullulan, HPMC E3, HPMC E5, HPMC E6, HPMC E15, HPMC K4M, Carbopol 940, PVP, Chitosan, Gelatin and PVA were used for preparation of FDF. Films with Pullulan and combination of HPMC E series showed transparent appearance, fast disintegration and dissolution. The prepared films were evaluated for their appearance, folding endurance, disintegration time....
In recent year due to advances in combinational chemistry and newer screening technique the large numbers of new drug candidates are synthesized fastly. Although the rate of discovery of newer drug is high, the major trouble in drug development technique is the poor solubility and bioavailability of drug molecule which gives rise to undesirable effect on dissolution rate and ultimately on absorption. A great deal of effort has been taken to resolve this problem. Among that the solid dispersion technique is one of the noteworthy techniques to improve bioavailability. But in practical point of view one should stumble upon large number of problems (Limitations) during enhancement of bioavailability and dissolution rate of poorly soluble drug by using solid dispersion method. The one of the imperative thing is that, these problems can be overcome by using some techniques. In this article we focused on the practical limitation / problems in solid dispersion technique and the methods to overcome them....
This article focus on the application of solid dispersion which helps to mask the bitter taste of drug as well improve its bioavailability. Solid dispersions have attracted considerable interest as an efficient means of improving the dissolution rate and enhance the bioavailability of a range of poorly water-soluble drugs (Biological Classification System BCS class-II ) as well as a method for masking the bitter taste of drugs. This article reviews the various preparation techniques for solid dispersion and also reviews application of nanoparticulate solid dispersion that have been reported recently as well some of ingredient which can be used to prepare Solid dispersion for improving bioavailability and masking the bitter taste of drug. Through drug nanoencapsulation, a higher content of drug may be delivered with less aggregation via placing the same drug mass in a greater number of tinier carriers. This leads to improve surface area for faster dissolution. This article also reviews various techniques for evaluation of solid dispersion...
In the present investigation an attempt was made for poorly soluble drug Repaglinide to form a solid dispersion both by solvent evaporation and spray drying method to improve dissolution rate, thus enhancing bio-availability of repaglinide, typically employed polymers like poloxamer 188, PVP-K-30, in varying ratio of 1:1, 1:3and 1:5 prepared by solvent evaporation. The formulation evaluated for in-vitro parameters like drug content and drug release. Based on the drug release formulation 1:1 ratio showed least solubility which was further formulated by Spray dried method using drug and poloxamer188, PVP-k-30 in the 1:1 ratio separately. The Spray dried formulation were carried out for drug content, drug release, FTIR, DSC, XRD, and SEM. Solid state characterization of drug–carrier 1:1 ratio for FTIR showed no any chemical compatibility between the drug and the polymer. Phase solubility studies revealed AL type for each carrier indicating linear increase in solubility with carrier concentration. Good uniformity of drug content was observed in ratios of 1:1, 1:3, 1:5 by solvent evaporation in the range from 85-99% and 1:1 ratio of spray drying showed the drug content ranges from 98-100%. All the solid dispersions showed dissolution improvement as compared to pure drug and physical mixture with faster drug release of 106 % with in 20 min for PVP-k-30 as compare with 104% release with 20 min for Poloxamer 188 this may be due to spray drying method. The stability study indicated that the solid dispersion of drug and carrier were remained stable for a period of 2 months. It was concluded that PVP k 30 is more effective in solubilizing Repaglinide in aqueous media as compared to Poloxamer 188....
Crystallization is the spontaneous arrangement of the particles into a repetitive orderly array, i.e., regular geometric patterns. Crystallization differs from precipitation in that the product is deposited from a supersaturated solution. Precipitation occurs when solutions of materials react chemically to form a product, which is sparingly soluble in the liquid and therefore deposits out. The formation of the crystals from solution involves three steps supersaturation, nucleus formation and crystal growth. Spherical crystallization is an agglomeration process that transforms crystals directly in to a compact spherical forms during the crystallization process. It is the versatile process that enables to control the type and the size of the crystals. It also enables co-precipitation of drug and encapsulating polymer in the form of spherical particle. Spherical crystallization can be successfully engineered when a suitable mixture of two or three partially miscible liquids is utilized as a crystallization solvent; this technique can be applied to a vast array of drugs and chemicals. Several steps including synthesis, crystallization, separation, and agglomeration can be combined into a single operation by employing spherical crystallization. This reduction in processing saves operating time and lowers production cost. The size of agglomerates can be easily controlled and the flowability and the compressibility of the granules can be improved so as to allow direct compression into tablets. If this process can be scaled-up to manufacturing level, this technology has the potential to provide the directly compressed spherical agglomerates with improving the physicochemical and micromeritic properties....
Paracetamol is an antipyretic drug which having 2 polymorphic forms, i.e. polymorph I (monoclinic form) and polymorph II (orthorhombic form). In market paracetamol polymorph I (monoclinic form) tablet is available. The main objective of studying different polymorphs of Paracetamol was to identify suitable polymorphic form for development of stable and effective dosage form and studying different physicochemical properties of Paracetamol polymorphs. Paracetamol polymorph study; developed orthorhombic polymorphic by using two different methods i.e. crystallization of orthorhombic paracetamol by melting monoclinic paracetamol and second method was preparing orthorhombic paracetamol by using an anhydrous nitrogen atmosphere. In that study second method was found to be suitable for developing orthorhombic polymorphic form on the basis of melting point study and PXRD study.IP Grade Paracetamol did not show result and then used USP Grade Paracetamol. By using USP Grade Paracetamol orthorhombic form was developed and comparative flow properties study of paracetamol polymorph carried out, in that orthorhombic form shows better flow properties and higher percentage of drug release after 30 minute....
Valganciclovir HCl is an antiviral drug. This was found in 2 polymorphic forms, i.e. amorphous and crystalline form. In market valganciclovir HCl crystalline form tablet is available, which is manufactured and marketed by Roche. And Roche having patent on valganciclovir HCl, which was approved on 29 march 2001 and patent expire on 29 march 2015. Many pharmaceutical company researches were going on valganciclovir HCL amorphous form tablet development. The main objective of studying different polymorphs of Valganciclovir HCl and Paracetamol was to identify suitable polymorphic form for development of stable and effective dosage form. Another objective to find out the suitable tablet preparation method for valganciclovir HCl semi-amorphous form. In preparation of valganciclovir HCl semi-amorphous form tablet was found that direct compression & wet-granulation method are not suitable method. Because after direct compression & wet-granulation semi-amorhous form converted into crystalline form. slugging method was most suitable method for development of valganciclovir HCl semi-amorphous tablet....
Controlled and sustained released formulations are widely used in modern era for the delivery of various ingredients. Oral sustained release product provides an advantage over conventional dosage form by optimizing biopharmaceutics, pharmacokinetic and pharmacodynamic properties of drug. The Sustained release formulation avoids frequents administration of the medicaments while maintaining a uniform and constants release rate of the active pharmaceutical ingredients over long period of time. Sustained release is a drug product formulation that provides the required dosage initially and then maintains or repeats it at desired intervals. Developing oral sustained release matrix tablets for drugs with constant release rate has always been a challenge to the pharmaceutical technologist. All pharmaceutical dosage forms contain many additives besides the active ingredients to assist manufacturing and to obtain the desired effect polymers have been successfully employed in the formulations to sustain the release of drug. Both the natural and synthetic polymers are employed in this process. Drug release through matrix system is determined by water penetration, polymer swelling, drug dissolution, drug diffusion and matrix erosion. Highly water soluble drugs are formulated as sustained release drug delivery system....
The aim of the present study is to formulation and evaluation of venlafaxine SR pellets. Venlafaxine is a novel anti-depressant used widely for treatment of generalised anxiety disorder but it is having disadvantage of having less biological half life of about 5 hrs due to extensive hepatic first pass metabolism. So in order to maintain the therapeutic concentration of venlafaxine for a prolonged period of time the SR tablets has been formulated. Hence, in the present the polymers such as Ethyl cellulose, Hydroxypropylmethylcellulose phthalate, EudragitRS100 were used as a coating polymer which helps in providing sustained release. The dissolution studies of the dosage form was performed and analysed by U.V spectrophotometer. Different evaluation parameters such as drug-excipient compatibility; in-vitro drug release was performed and showed acceptable as per pharmacopoeial specification. Different polymers are optimized on the basis of release pattern. The present research work was directed towards the development of a sustained release dosage form of venlafaxine in the form of capsules to be taken once daily. The marketed formulation was evaluated for the in-vitro release studied and formulated product is compared with the marketed product extended release pellets....
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